Synthesis and cytotoxicity of analogues of the antibiotic BE 10988 inhibitors of DNA topoisomerase II

Bioorg Med Chem Lett. 1999 Jul 19;9(14):2025-30. doi: 10.1016/s0960-894x(99)00307-8.

Abstract

Indolequinone derivatives of the antitumour antibiotic BE 10988 were synthesized and evaluated for their cytotoxicity and action mechanism. The quinone system is essential to biological activity and the thiazole ring plays a major role in the poisoning of topoisomerase II.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Division / drug effects
  • DNA / metabolism
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / metabolism
  • Enzyme Inhibitors / pharmacology*
  • Indoles / chemistry
  • Inhibitory Concentration 50
  • Leukemia L1210 / drug therapy
  • Mice
  • Quinones / chemistry
  • Solubility
  • Structure-Activity Relationship
  • Thiazoles / chemistry*
  • Topoisomerase II Inhibitors*

Substances

  • Enzyme Inhibitors
  • Indoles
  • Quinones
  • Thiazoles
  • Topoisomerase II Inhibitors
  • BE 10988
  • DNA